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Assay Detail

CHEMBL4670928

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Inhibiton of EGFR (unknown origin) expressed in human A431 cells assessed as reduction in EGFR induced cell viability after 96 hrs by CellTiter-Glo assay
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type A-431
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Epidermal growth factor receptor (CHEMBL203)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Targeting Her2-insYVMA with Covalent Inhibitors-A Focused Compound Screening and Structure-Based Design Approach.
Lategahn J,Hardick J,Grabe T,Niggenaber J,Jeyakumar K,Keul M,Tumbrink HL,Becker C,Hodson L,Kirschner T,Klövekorn P,Ketzer J,Baumann M,Terheyden S,Unger A,Weisner J,Müller MP,van Otterlo WAL,Bauer S,Rauh D
J Med Chem (2020) 63 : 11725 -11755
PubMed 32931277 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 5.72 6.06

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4757145 1 6.06
CHEMBL3353410 OSIMERTINIB 4.0 1 6.04
CHEMBL1173655 AFATINIB 4.0 1 5.85
CHEMBL4795165 1 5.80
CHEMBL4787483 1 5.78
CHEMBL4756368 1 5.65
CHEMBL554 LAPATINIB 4.0 1 5.57
CHEMBL180022 NERATINIB 4.0 1 5.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4757145 IC50 = 862.0 nM 6.06
CHEMBL3353410 OSIMERTINIB IC50 = 911.0 nM 6.04
CHEMBL1173655 AFATINIB IC50 = 1401.0 nM 5.85
CHEMBL4795165 IC50 = 1570.0 nM 5.80
CHEMBL4787483 IC50 = 1675.0 nM 5.78
CHEMBL4756368 IC50 = 2236.0 nM 5.65
CHEMBL554 LAPATINIB IC50 = 2685.0 nM 5.57
CHEMBL180022 NERATINIB IC50 = 10117.0 nM 5.00